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Formula | C22H18N4OS |
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Molecular Weight | 386.47 | CAS No. | 319460-85-0 | |
Solubility (25°C)* | In vitro | DMSO | 26 mg/mL (67.27 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. | |||||||||||
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In vitro | Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2] | |||||||||||
In vivo | Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma. | |||||||||||
Features | Superior as second-line therapy relative to sorafenib (current standard-of-care). |
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Data from [J Biomol Screen, 2011, 16, 141-154]
, , Oncogene, 2017, 36(36):5098-5109
, , Dr. Cheri Pasch of UW Madison
Data from [Data independently produced by , , J Biomol Screen, 2011,16: 141-154]
Hematopoietic-specific heterozygous loss of Dnmt3a exacerbates colitis-associated colon cancer [ J Exp Med, 2023, 220(11)e20230011] | PubMed: 37615936 |
Hematopoietic-specific heterozygous loss of Dnmt3a exacerbates colitis-associated colon cancer [ J Exp Med, 2023, 220(11)e20230011] | PubMed: 37615936 |
Single-cell RNA sequencing identifies critical transcription factors of tumor cell invasion induced by hypoxia microenvironment in glioblastoma [ Theranostics, 2023, 13(11):3744-3760] | PubMed: 37441593 |
SMARCB1 regulates the hypoxic stress response in sickle cell trait [ Proc Natl Acad Sci U S A, 2023, 120(21):e2209639120] | PubMed: 37186844 |
Selective induction of human renal interstitial progenitor-like cell lineages from iPSCs reveals development of mesangial and EPO-producing cells [ Cell Rep, 2023, S2211-1247(23)01614-5] | PubMed: 38237600 |
Microenvironmental control of hematopoietic stem cell fate via CXCL8 and protein kinase C [ Cell Rep, 2023, 42(5):112528] | PubMed: 37209097 |
A subset of VEGFR-TKIs activates AMPK in LKB1-mutant lung cancer [ Cancer Sci, 2023, 114(4):1651-1662] | PubMed: 36459496 |
Potential therapeutic target secretogranin II might cooperate with hypoxia-inducible factor 1α in sunitinib-resistant renal cell carcinoma [ Cancer Sci, 2023, 10.1111/cas.15914] | PubMed: 37545017 |
Potential therapeutic target secretogranin II might cooperate with hypoxia-inducible factor 1α in sunitinib-resistant renal cell carcinoma [ Cancer Sci, 2023, 114(10):3946-3956] | PubMed: 37545017 |
Sphingosine-1-phosphate derived from PRP-Exos promotes angiogenesis in diabetic wound healing via the S1PR1/AKT/FN1 signalling pathway [ Burns Trauma, 2023, 11:tkad003] | PubMed: 37251708 |
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